Cook et al. (2005, 2010) reported the synthesis method of bis-β-carboline of 6-alkynyl bridge connection, subsequently confirmed that such bis-β-carboline alkaloids has a good affinity on benzodiazepine receptor (Bz) and γ-aminobutyric acid (GABA) receptor.
Winckler et al. (2010) designed the bis-3,4-dihydro-β-carboline and bis-β-carboline compounds of two methylene bridge connecting and 9-methylene bridge connecting, and demonstrated that these compounds have better inhibitory activity on acetylcholinesterase and butyrylcholinesterase
Zheng et al. synthesized bis-3,4-dihydro-β-carboline and bis-β-carboline compound of the 9-methylene bridge connecting and 11C-labeled according to the synthesis methods of Winckler et al, and found that such bis-β-carboline compounds can be used as a new imaging agent of the positive radiation tomography for acetylcholinesterase imaging in Alzheimer's disease (AD) patient, but the role of these compounds in anti-tumor were not disclosed.

The bis-β-carboline reported in the literature was bridge connected in the 1 position.

The bis-β-carboline reported in the literature was bridge connected in the 6 position.

The bis-β-carboline reported in the literature was bridge connected in the 2 position.

The bis-β-carboline reported in the literature was bridge connected in the 9 position.